PRALSETINIB


Synonyms	BLU-123244 BLU-667 BLU123244 Blu-667 Gavreto Pralsetinib X-581238 X581238
Status
Molecule Category	Free-form
UNII	1WPE73O1WV


InChI Key	GBLBJPZSROAGMF-RWYJCYHVSA-N
Smiles	CO[C@]1(C(=O)N[C@@H](C)c2ccc(-n3cc(F)cn3)nc2)CC[C@H](c2nc(C)cc(Nc3cc(C)[nH]n3)n2)CC1
InChI	InChI=1S/C27H32FN9O2/c1-16-11-22(33-23-12-17(2)35-36-23)34-25(31-16)19-7-9-27(39-4,10-8-19)26(38)32-18(3)20-5-6-24(29-13-20)37-15-21(28)14-30-37/h5-6,11-15,18-19H,7-10H2,1-4H3,(H,32,38)(H2,31,33,34,35,36)/t18-,19-,27+/m0/s1

Mechanism of Action	Action	Reference
Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET inhibitor	INHIBITOR	FDA

Targets	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase JakA family	-	2	-	-	-
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase JakB family	-	2	-	-	-
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase PDGFR family	-	6.5	-	-	-
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase Ret family	-	0.7-1.93	-	-	-

	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Homo sapiens	-	0.7-6.5	-	-	-
Mus musculus	-	17	-	-	-


Protein: Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET Description: Proto-oncogene tyrosine-protein kinase receptor Ret Organism : Homo sapiens P07949 ENSG00000165731













Protein: Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET Description: Proto-oncogene tyrosine-protein kinase receptor Ret Organism : Homo sapiens P07949 ENSG00000165731













Protein: Tyrosine-protein kinase receptor RET Description: Proto-oncogene tyrosine-protein kinase receptor Ret Organism : Homo sapiens P07949 ENSG00000165731













Protein: Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET Description: Kinesin-1 heavy chain Organism : Homo sapiens P33176 ENSG00000170759













Protein: Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET Description: Coiled-coil domain-containing protein 6 Organism : Homo sapiens Q16204 ENSG00000108091

CONTENTS